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Cat. No.: HY-146209

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Tubulin polymerization-IN-13

Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC₅₀=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity.

For research use only. We do not sell to patients.

CAS No.: 2426665-56-5
Formula: C₂₀H₂₁NO₆
Molecular Weight:371.38

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (282 KB)

Tubulin polymerization-IN-13 Chemical Structure

CAS No.: 2426665-56-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 0.37 μM (tubulin polymerization)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Astrocyte	GI₅₀	>10 μM Compound: 4f	Cytotoxicity against normal human astrocytes assessed as inhibition of cell growth Cytotoxicity against normal human astrocytes assessed as inhibition of cell growth	[PMID: 32417696]
Daoy	IC₅₀	0.005 nM Compound: 4f	Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth Antiproliferative activity against human Daoy cells assessed as inhibition of cell growth	[PMID: 32417696]
HeLa	IC₅₀	2.8 nM Compound: 4f	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth	[PMID: 32417696]
HL-60	IC₅₀	2.7 nM Compound: 4f	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth	[PMID: 32417696]
HT-29	IC₅₀	2.1 nM Compound: 4f	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth	[PMID: 32417696]
Jurkat	IC₅₀	0.28 nM Compound: 4f	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth	[PMID: 32417696]
PBL	GI₅₀	>10 μM Compound: 4f	Cytotoxicity against PHA-stimulated human PBL assessed as inhibition of cell growth Cytotoxicity against PHA-stimulated human PBL assessed as inhibition of cell growth	[PMID: 32417696]
PBL	GI₅₀	8.7 μM Compound: 4f	Cytotoxicity against human PBL assessed as inhibition of cell growth Cytotoxicity against human PBL assessed as inhibition of cell growth	[PMID: 32417696]
SEM	IC₅₀	0.31 nM Compound: 4f	Antiproliferative activity against human SEM cells assessed as inhibition of cell growth Antiproliferative activity against human SEM cells assessed as inhibition of cell growth	[PMID: 32417696]

In Vitro

Tubulin polymerization-IN-13 (0.005-2.8 nM) treatment inhibits tumor cell proliferation^[1].
Tubulin polymerization-IN-13 (8.7-10 μM) is non-toxic in non-tumor cells^[1].
Tubulin polymerization-IN-13 (1-50 nM; 24 h) treatment induces cell cycle arrest in G2/M^[1].
Tubulin polymerization-IN-13 (10 nM; 24 and 48 h) treatment induces cell apoptosis^[1].
Tubulin polymerization-IN-13 (10-100 nM; 24 h) treatment induces alteration of the microtubule network^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells
Concentration:

0.005-2.8 nM
Incubation Time:
Result:

Showed IC₅₀s of 2.8 nM, 2.1 nM, 0.005 nM, 2.7 nM, 0.31 nM, and 0.28 nM for HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells, respectively.

Cell Cytotoxicity Assay^[1]

Cell Line:

Peripheral blood lymphocytes (PBL)
Concentration:

8.7-10 μM
Incubation Time:
Result:

Showed a GI₅₀ of 8.7 μM in quiescent lymphocytes.

Cell Cycle Analysis^[1]

Cell Line:

HeLa cells
Concentration:

1, 5, 10, and 50 nM
Incubation Time:

24 hours
Result:

Induced a G2/M arrest at 10 nM, increased G2/M cells accompanied by a strong reduction of cells in the G1 phase.

Apoptosis Analysis^[1]

Cell Line:

HeLa cells
Concentration:

10 nM
Incubation Time:

24 and 48 hours
Result:

Induced caspase-9 activation, PARP cleavage, Bcl-2 phosphorylation and Mcl-1 downregulation.

Immunofluorescence^[1]

Cell Line:

HeLa cells
Concentration:

10, 50, and 100 nM
Incubation Time:

24 hours
Result:

Showed the disorganization of microtubules at 10 nM, and much more evident at 50 and 100 nM.

In Vivo

Tubulin polymerization-IN-13 (intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times) reduces tumor growth in a dose-dependent manner in an orthotopic murine tumor model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Seven-week-old C57BL/6 female mice orthotopically injected into the mammary fat pad with E0771 mammary carcinoma cells^[1]
Dosage:

15 or 5 mg/kg
Administration:

Intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times
Result:

Reduced tumor mass by 45.7% and 16.9% at 15 and 5 mg/kg, respectively.
Showed no sign of toxicity and no decreasement in animal body weight.

Chemical Information

CAS No. 2426665-56-5
Molecular Weight 371.38
Formula C₂₀H₂₁NO₆
SMILES

CCOC1=CC2=C(C(C(C3=CC(OC)=C(C(OC)=C3)OC)=O)=C(O2)N)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Paola Oliva, et al. Design, synthesis, in vitro and in vivo biological evaluation of 2-amino-3-aroylbenzo[b]furan derivatives as highly potent tubulin polymerization inhibitors. Eur J Med Chem. 2020 Aug 15;200:112448. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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